ZA201207727B - Morpholinylquinazolines - Google Patents

Morpholinylquinazolines

Info

Publication number
ZA201207727B
ZA201207727B ZA2012/07727A ZA201207727A ZA201207727B ZA 201207727 B ZA201207727 B ZA 201207727B ZA 2012/07727 A ZA2012/07727 A ZA 2012/07727A ZA 201207727 A ZA201207727 A ZA 201207727A ZA 201207727 B ZA201207727 B ZA 201207727B
Authority
ZA
South Africa
Prior art keywords
morpholinylquinazolines
Prior art date
Application number
ZA2012/07727A
Inventor
Werner Mederski
Frank Zenke
Thomas Fuchss
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to DE102010011493 priority Critical
Priority to PCT/EP2011/000767 priority patent/WO2011113512A1/en
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of ZA201207727B publication Critical patent/ZA201207727B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
ZA2012/07727A 2010-03-16 2012-10-15 Morpholinylquinazolines ZA201207727B (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
DE102010011493 2010-03-16
PCT/EP2011/000767 WO2011113512A1 (en) 2010-03-16 2011-02-17 Morpholinylquinazolines

Publications (1)

Publication Number Publication Date
ZA201207727B true ZA201207727B (en) 2013-06-26

Family

ID=43828057

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2012/07727A ZA201207727B (en) 2010-03-16 2012-10-15 Morpholinylquinazolines

Country Status (16)

Country Link
US (1) US9126952B2 (en)
EP (1) EP2547664B1 (en)
JP (1) JP2013522249A (en)
KR (1) KR20130017086A (en)
CN (1) CN102803227B (en)
AR (1) AR080757A1 (en)
AU (1) AU2011229542A1 (en)
BR (1) BR112012022868A2 (en)
CA (1) CA2793299A1 (en)
EA (1) EA201201289A1 (en)
ES (1) ES2586227T3 (en)
IL (1) IL221901A (en)
MX (1) MX2012010557A (en)
SG (1) SG183855A1 (en)
WO (1) WO2011113512A1 (en)
ZA (1) ZA201207727B (en)

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EP2841428B1 (en) 2012-04-24 2018-08-22 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
JP6360878B2 (en) 2013-03-12 2018-07-18 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated DNA-PK inhibitor
UY35464A (en) 2013-03-15 2014-10-31 Araxes Pharma Llc KRAS G12C covalent inhibitors.
DE102013008118A1 (en) 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
EP3636639A1 (en) * 2013-10-10 2020-04-15 Araxes Pharma LLC Inhibitors of kras g12c
TWI659021B (en) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Inhibitors of kras g12c
LT3424920T (en) 2013-10-17 2020-08-10 Vertex Pharmaceuticals Incorporated Co-crystals of (s)-n-methyl-8-(1-((2`-methyl-[4,5`-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors
TWI694837B (en) 2014-09-18 2020-06-01 美商亞瑞克西斯製藥公司 Combination therapies for treatment of cancer
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
KR20180005178A (en) 2015-04-10 2018-01-15 아락세스 파마 엘엘씨 Substituted quinazoline compounds and methods for their use
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2018533939A (en) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Method for screening for inhibitors of RAS
MX2018005967A (en) 2015-11-16 2018-08-29 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof.
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CN110036010A (en) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 The inhibitor of KRAS G12C mutain
CN110312711A (en) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 Heterocyclic compound and its application method as RAS inhibitor
WO2018218070A2 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Covalent inhibitors of kras
JP2020521741A (en) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー Compounds for the treatment of cancer and methods of their use
EP3551188A1 (en) * 2017-10-31 2019-10-16 Southern Research Institute Substituted quinazoline sulfonamides as thioredoxin interacting protein (txnip) inhibitors
WO2020148403A1 (en) 2019-01-17 2020-07-23 Universite De Lille 5-membered heteroaryl compounds containing a hydroxamate moiety and their use

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Also Published As

Publication number Publication date
SG183855A1 (en) 2012-10-30
IL221901A (en) 2016-04-21
US9126952B2 (en) 2015-09-08
CA2793299A1 (en) 2011-09-22
US20130012489A1 (en) 2013-01-10
AU2011229542A1 (en) 2012-11-08
KR20130017086A (en) 2013-02-19
JP2013522249A (en) 2013-06-13
BR112012022868A2 (en) 2018-06-05
ES2586227T3 (en) 2016-10-13
CN102803227B (en) 2016-01-20
MX2012010557A (en) 2012-10-05
IL221901D0 (en) 2012-12-02
AR080757A1 (en) 2012-05-09
EP2547664A1 (en) 2013-01-23
EP2547664B1 (en) 2016-05-04
EA201201289A1 (en) 2013-08-30
WO2011113512A1 (en) 2011-09-22
CN102803227A (en) 2012-11-28

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